JPH10114650A - Improver for aqueous body fluid and composition for oral administration comprising the same - Google Patents

Improver for aqueous body fluid and composition for oral administration comprising the same

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Publication number
JPH10114650A
JPH10114650A JP8272726A JP27272696A JPH10114650A JP H10114650 A JPH10114650 A JP H10114650A JP 8272726 A JP8272726 A JP 8272726A JP 27272696 A JP27272696 A JP 27272696A JP H10114650 A JPH10114650 A JP H10114650A
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JP
Japan
Prior art keywords
action
represented
group
general formula
embedded image
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Granted
Application number
JP8272726A
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Japanese (ja)
Other versions
JP4049406B2 (en
Inventor
Masanori Kosuge
正規 小菅
Takuo Kosuge
卓夫 小菅
Makoto Fukushima
信 福島
Yasunori Inaoka
靖規 稲岡
Takehiro Okuda
剛弘 奥田
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
DOKUTAAZU KOSUMETEIKUSU KK
Pola Chemical Industries Inc
Original Assignee
DOKUTAAZU KOSUMETEIKUSU KK
Pola Chemical Industries Inc
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Application filed by DOKUTAAZU KOSUMETEIKUSU KK, Pola Chemical Industries Inc filed Critical DOKUTAAZU KOSUMETEIKUSU KK
Priority to JP27272696A priority Critical patent/JP4049406B2/en
Publication of JPH10114650A publication Critical patent/JPH10114650A/en
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Publication of JP4049406B2 publication Critical patent/JP4049406B2/en
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Expired - Lifetime legal-status Critical Current

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  • Coloring Foods And Improving Nutritive Qualities (AREA)
  • Cosmetics (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

Abstract

PROBLEM TO BE SOLVED: To prepare the subject improver, comprising a specific compound, capable of stimulating secretory organs and promoting and improving actions of aqueous body fluids (water), useful as a composition for oral administration such as a food or a medicine and having skin beautifying actions, etc. SOLUTION: This improver for aqueous body fluids (water) comprises a compound represented by formula I [R1 is OH or a saccharide residue; R2 is H, OH, hydroxymethyl or carboxyl; R3 is methyl, carboxyl or H; A is carbonyl or CH-R4 (R4 is a caccharide residue, etc.)] and/or its physiologically permissible salt. The compound is preferably emodine represented by formula II, aloe emodin represented by formula III, rhein, etc., represented by formula IV. For example, the daily dose thereof for an adult is preferably 1-10,000mg orally administered in one to several divided portions at the time of administration.

Description

【発明の詳細な説明】DETAILED DESCRIPTION OF THE INVENTION

【０００１】[0001]

【発明の属する技術分野】本発明は、津液作用の改善効
果を有する津液改善剤、及びそれを含有する食品、医薬
等の経口投与用組成物に関する。BACKGROUND OF THE INVENTION 1. Field of the Invention The present invention relates to an agent for improving tsunami which has an effect of improving the effect of tsunami, and a composition containing the same for oral administration of foods, medicines and the like.

【０００２】[0002]

【従来の技術】漢方思想における気、血、水の考え方
は、その薬理作用の捉え方のユニークさと、漢方薬選択
時の合理的な指標であるために、古くより研究されてき
た。これらの内、気、血の意味するものについては、多
くのことが解明されてきた。例えば、血とは酸素、栄養
等エネルギーを中心とする補給・代謝を表すキーワード
であり、気とは生命活動の恒常性機構の活動状況と生命
活動の原動力の状況を表すキーワードであることが知ら
れている。2. Description of the Related Art The concept of qi, blood, and water in Chinese medicine has long been studied because of its uniqueness in understanding its pharmacological action and a rational index for selecting Chinese medicine. Of these, many have been elucidated about the meanings of qi and blood. For example, it is known that blood is a keyword that represents the supply and metabolism mainly of energy such as oxygen and nutrition, and ki is a keyword that represents the status of the homeostasis of life activity and the status of the driving force of life activity. Have been.

【０００３】しかし、水（津液）の働きについては老廃
物の代謝・***作用のみしか知られておらず、気・血・
水の論理体型において遅れて認識された為、その真の作
用（津液作用）の解明は未完であった。また、津液作用
と現代医学で認識されている種々の薬理作用等との関係
や津液の現代医学における役割などはあまり知られてお
らず、現代医学の分野における津液作用の解明及び津液
作用の改善をもたらす食品や医薬等の開発が望まれてい
た。[0003] However, only the metabolism and excretion of waste products is known for the function of water (tsu liquor).
Since the recognition was delayed in the logical form of water, the elucidation of its true action (Tsukumi action) was incomplete. Also, little is known about the relationship between the pulp action and the various pharmacological actions recognized in modern medicine, and the role of pulp in modern medicine. The development of foods, medicines, etc. that bring about this has been desired.

【０００４】[0004]

【発明が解決しようとする課題】本発明は、このような
状況を踏まえてなされたものであり、津液の真の作用を
明らかにし、津液作用を改善しうる物質及びそれを含有
する食品、医薬等の経口投与用組成物を提供することを
課題とする。DISCLOSURE OF THE INVENTION The present invention has been made in view of such circumstances, and has been made to clarify the true action of tsuju, to improve the tsuju action, and to provide foods and pharmaceuticals containing the same. It is an object to provide a composition for oral administration such as

【０００５】[0005]

【課題を解決するための手段】本発明者等は、このよう
な状況に鑑み、津液の真の作用を求めて鋭意研究を重ね
た結果、津液作用が、ある種の物質の働きによって水分
の体外への分泌を司る器官を刺激し、体内水分の体外へ
の分泌を促進させる作用を意味していることを見出し
た。そして、そのような分泌器官を刺激し津液作用を促
進・改善しうる物質である津液改善剤をスクリーニング
することにより、本発明を完成した。Means for Solving the Problems In view of such a situation, the present inventors have conducted intensive studies in search of the true function of tsuju. It has been found that it has an effect of stimulating organs responsible for secretion outside the body and promoting secretion of body water outside the body. Then, the present invention was completed by screening for a tsumuco-ameliorating agent, which is a substance capable of stimulating such secretory organs and promoting / improving the action of tsuku.

【０００６】すなわち、本発明は、下記一般式（Ｉ）で
表される化合物及び／又はその生理的に許容される塩か
らなる津液改善剤を提供するものである。。[0006] That is, the present invention provides a tsutsumitsu-improving agent comprising a compound represented by the following general formula (I) and / or a physiologically acceptable salt thereof. .

【０００７】[0007]

【化７】 Embedded image

【０００８】［式（Ｉ）中、Ｒ1は水酸基又は糖残基を
表し、Ｒ2は水素原子、水酸基、ヒドロキシメチル基又
はカルボキシル基を表し、Ｒ3はメチル基、カルボキシ
ル基又は水素原子を表す。Ａはカルボニル基又はＣＨ−
Ｒ4で表される基を表す。ここでＲ4は糖残基又は置換基
を有してもよいアントラニル基を表す。］[In the formula (I), R 1 represents a hydroxyl group or a sugar residue, R 2 represents a hydrogen atom, a hydroxyl group, a hydroxymethyl group or a carboxyl group, and R 3 represents a methyl group, a carboxyl group or a hydrogen atom. Represent. A is a carbonyl group or CH-
Represents a group represented by R 4 . Here, R 4 represents a sugar residue or an anthranyl group which may have a substituent. ]

【０００９】また、本発明は、前記津液改善剤を含有す
る経口投与用組成物を提供するものである。[0009] The present invention also provides a composition for oral administration containing the above-mentioned agent for improving tsuku.

【００１０】本発明の津液改善剤とは、水分の体外への
分泌を司る器官を刺激して体内水分の体外への分泌を促
し津液作用を促進・改善する作用、すなわち津液改善作
用を有する物質をいう。本発明者らは、津液作用が真皮
から表皮への水分分泌を促進し表皮に十分な水分を保持
させることによって起こる美肌作用、アトピー性皮膚
炎、湿疹、皮膚真菌症、疣贅、色素沈着症、尋常性乾
癬、老人性乾皮症、老人性角化腫、火傷等の各種皮膚疾
患治療作用、発毛促進作用、発汗促進作用、胃壁、腎
臓、腸管等での水分分泌を促進させることによって起こ
る消化液分泌促進作用、利尿作用、便通促進作用にかか
わる作用であることを見出した。すなわち、漢方生薬の
薬効分類を詳細に検討し、現代医薬分類との対比を行っ
た結果、水（津液）が関与すると言われているしゃ下、
利水、消導、補陰と言った薬草群の作用が現代医薬品分
類における美肌作用、アトピー性皮膚炎、湿疹、皮膚真
菌症、疣贅、色素沈着症、尋常性乾癬、老人性乾皮症、
老人性角化腫、火傷等の各種皮膚疾患の治療作用、発毛
促進作用、消化液分泌促進作用、発汗促進作用、利尿作
用、便通促進作用と係わりが深いことを見出した。[0010] The agent of the present invention is a substance having an effect of stimulating the organs responsible for the secretion of water to the outside of the body to promote the secretion of water from the body to the outside of the body to promote and improve the effect of the tsuku, ie a substance having the action of improving the tsuku. Say. The present inventors have proposed a tanning effect that promotes the secretion of water from the dermis to the epidermis and retains sufficient water in the epidermis, a beautiful skin effect, atopic dermatitis, eczema, dermatomycosis, warts, and pigmentation. By treating various skin diseases such as psoriasis vulgaris, senile xeroderma, senile keratomas and burns, promoting hair growth, promoting sweating, and promoting water secretion in the stomach wall, kidneys, intestinal tract, etc. It has been found that the action is related to the digestive juice secretion promoting action, diuretic action, and bowel movement promoting action that occur. In other words, after examining the medicinal classification of Chinese herbal medicine in detail and comparing it with the modern medicine classification, it is said that water (Tsui) is involved,
The effects of herbal medicines such as irrigation, guidance, and prosthesis are the skin effects in modern medicine classification, atopic dermatitis, eczema, dermatomycosis, warts, pigmentation, psoriasis vulgaris, senile xerosis,
It has been found that it is closely related to the treatment of various dermatological diseases such as senile keratoma and burns, hair growth promotion, digestive secretion promotion, sweat perspiration, diuresis, and bowel movement.

【００１１】この知見をもとに種々の物質について美肌
作用、アトピー性皮膚炎治療作用、湿疹の治療作用、発
毛促進作用、消化液分泌促進作用、発汗促進作用を指標
にスクリーニングを重ねたところ、上記一般式（Ｉ）で
表される化合物及び／又はその生理的に許容される塩が
このような作用に優れることを見いだしたものである。Based on this finding, screening was carried out on various substances based on the beautifying action, atopic dermatitis treating action, eczema treating action, hair growth promoting action, digestive juice secretion promoting action, and sweat promoting action on various substances. It has been found that the compound represented by the above general formula (I) and / or a physiologically acceptable salt thereof are excellent in such action.

【００１２】上記一般式（Ｉ）で表される化合物及び／
又はその生理的に許容される塩は、経皮吸収促進作用、
肝機能の改善や免疫機能の改善作用等を有していること
は知られているものの、それが真の意味での津液改善作
用を有することは知る余地もなかった。更に、一般式
（Ｉ）で表される化合物及び／又はその生理的に許容さ
れる塩が美肌作用、アトピー性皮膚炎、湿疹、皮膚真菌
症、疣贅、色素沈着症、尋常性乾癬、老人性乾皮症、老
人性角化腫、火傷等の皮膚疾患治療作用、発毛促進作
用、発汗促進作用、消化液分泌促進作用、利尿作用、便
通促進作用を有することは全く知られていなかった。The compound represented by the general formula (I) and / or
Or a physiologically acceptable salt thereof has a transdermal absorption promoting action,
Although it is known to have an effect of improving liver function and immune function, there is no way to know that it has a true effect of improving tsukusu. Further, the compound represented by the general formula (I) and / or a physiologically acceptable salt thereof may be used as a skin beautifier, atopic dermatitis, eczema, dermatomycosis, warts, pigmentation, psoriasis vulgaris, elderly people It has never been known to have a skin xeroderma, senile keratoma, skin wound treatment such as burns, a hair growth promoting action, a sweat promoting action, a digestive juice secretion promoting action, a diuretic action, and a bowel movement promoting action. .

【００１３】[0013]

【発明の実施の形態】以下に、本発明の実施の形態を説
明する。 （１）本発明の津液改善剤 本発明の津液改善剤は、上記一般式（Ｉ）で表される化
合物及び／又はその生理的に許容される塩からなる。Embodiments of the present invention will be described below. (1) Tsutsumi-improving agent of the present invention The tsumumo-improving agent of the present invention comprises the compound represented by the above general formula (I) and / or a physiologically acceptable salt thereof.

【００１４】ここで、式（Ｉ）中、Ｒ1は水酸基又は糖
残基を表し、Ｒ2は水素原子、水酸基、ヒドロキシメチ
ル基又はカルボキシル基を表し、Ｒ3はメチル基、カル
ボキシル基又は水素原子を表す。Ａはカルボニル基又は
ＣＨ−Ｒ4で表される基を表し、Ｒ4は糖残基又は置換基
を有してもよいアントラニル基を表す。Here, in the formula (I), R 1 represents a hydroxyl group or a sugar residue, R 2 represents a hydrogen atom, a hydroxyl group, a hydroxymethyl group or a carboxyl group, and R 3 represents a methyl group, a carboxyl group or a hydrogen group. Represents an atom. A represents a group represented by a carbonyl group or a CH-R 4, R 4 denote an anthranyl group which may have a sugar residue or a substituent.

【００１５】このような化合物として具体的には、下記
一般式（ＩＩ）で表されるエモジン、下記一般式（ＩＩ
Ｉ）で表されるアロエエモジン、下記一般式（ＩＶ）で
表されるライン、下記一般式（Ｖ）で表されるセンノサ
イド、又は下記一般式（ＶＩ）で表されるアロインが挙
げられる。尚、一般式（Ｖ）中、ＧｌＯ又はＯＧｌは糖
残基を表わす。Specific examples of such a compound include emodin represented by the following general formula (II) and emodin represented by the following general formula (II)
Examples include aloe-emodin represented by I), a line represented by the following general formula (IV), sennoside represented by the following general formula (V), and aloin represented by the following general formula (VI). In general formula (V), GlO or OGl represents a sugar residue.

【００１６】[0016]

【化８】 Embedded image

【００１７】[0017]

【化９】 Embedded image

【００１８】[0018]

【化１０】 Embedded image

【００１９】[0019]

【化１１】 Embedded image

【００２０】[0020]

【化１２】 Embedded image

【００２１】また、上記化合物の生理的に許容される塩
とは、例えば、ナトリウム、カリウム等のアルカリ金属
塩、カルシウム、マグネシウム等のアルカリ土類金属
塩、アンモニウム塩、トリエチルアミンやトリエタノー
ルアミン等の有機アミン塩、リジンやアルギニン等の塩
基性アミノ酸塩等が好ましく例示できる。これらの対塩
基は１種でも２種以上を組み合わせて用いても構わな
い。The physiologically acceptable salts of the above compounds include, for example, alkali metal salts such as sodium and potassium, alkaline earth metal salts such as calcium and magnesium, ammonium salts, and triethylamine and triethanolamine. Preferred examples include organic amine salts and basic amino acid salts such as lysine and arginine. These counterbases may be used alone or in combination of two or more.

【００２２】一般式（Ｉ）で表される化合物及び／又は
その生理的に許容される塩は何れも市販されており入手
可能である。本発明の上記化合物からなる津液改善剤
は、津液作用を促進・改善する効果を有する。津液作用
は、その発現形態としてしゃ下作用、利水作用、補陰作
用、消導作用として生体に発現することが知られてい
る。これらの作用を有する漢方生薬としては、しゃ下作
用であれば、ダイオウ、バンシャヨウ、ロカイ、マシニ
ン、ケンゴシ、カンスイ、ゲンカ、ゾクズイシ、ウキュ
ウコンピ等が知られており、利水作用を有する漢方生薬
としては、チョレイ、ブクリョウ、タクシャ、インチン
コウ、ヨクイニン、トウカニン、ジフシ、トウキヒ、キ
ンセンソウ等が知られており、補陰作用を有する漢方生
薬としては、シャジン、セイヨウジン、テンモンドウ、
バクモンドウ、セッコク、ギョクチク、ヒャクゴウ、ソ
ウキセイ、カンレンソウ、ジョテイシ、ゴマ、コクズ、
キバン、ベッコウ等が知られており、消導作用を有する
漢方生薬としては、サンザシ、クレンコンピ、ヒシ、カ
クシツ、ライガン、ビンロウジ、ナンカシ、タイサン等
が知られている。The compound represented by the general formula (I) and / or a physiologically acceptable salt thereof are all commercially available. The Tsutsumi improver comprising the above compound of the present invention has an effect of promoting and improving the action of Tsutsumi. It is known that the tsuju action is expressed in a living body as a mode of expression, such as a shampooing action, a water-supplying action, a prosthesis action, and a conduction action. As a herbal crude drug having these effects, if it is a shampooing effect, rhubarb, banshayou, rokai, machinin, kengoshi, Kansui, Genka, Zokuzuishi, kyukyu compi, etc. Chorei, Bokuryo, Takusha, Inchinko, Jokuinin, Toukanin, Difushi, Tokhihi, Kinsenso and the like are known, and as herbal crude drugs having a prominence action, Shajin, Chinese ginseng, Tenmondou,
Bakumondou, Seckkoku, Arctic, Antelope, Sukikisei, Kanrensou, Joteishi, Sesame, Kokuzu,
Kiban, bekko, and the like are known, and as a Chinese herbal medicine having a deconducting action, hawthorn, krencompi, hishi, kakushitsu, reigan, areca, nankashi, and taisan are known.

【００２３】これらについて文献等を調べてみると、美
肌作用、発毛促進作用、抗アレルギー作用、抗炎症作
用、消化促進作用等の薬理作用が重複していることが見
出された。ここに本発明者等は注目し、「水」（津液）
の作用は現代医学における美肌作用、アトピー性皮膚炎
治療作用、発毛促進作用、湿疹の治療作用、消化液分泌
促進作用、発汗促進作用、利尿作用、便通促進作用等を
指標とすることができることを見出した。尚、これらの
作用の一つを有する物質は、大なり小なり他の作用も有
している場合が多い。したがって、これらの作用の一つ
を指標にするスクリーニングを行えば、他の作用の推定
を行うこともできる。Examination of the literature and the like reveals that pharmacological actions such as a skin beautiful action, a hair growth promoting action, an anti-allergic action, an anti-inflammatory action, and a digestive promoting action are duplicated. Here, the present inventors pay attention, and consider "water" (Tsu liquid).
The action of can be used as an index of the beautiful skin action, atopic dermatitis treatment action, hair growth promotion action, eczema treatment action, digestive secretion promotion action, sweat perspiration action, diuretic action, bowel movement promotion action, etc. in modern medicine. Was found. In addition, substances having one of these actions often have other actions to a greater or lesser degree. Therefore, if screening is performed using one of these actions as an index, other actions can be estimated.

【００２４】本発明の津液改善剤は、美肌作用、アトピ
ー性皮膚炎治療作用、湿疹で代表される皮膚炎群治療作
用、皮膚真菌症治療作用、疣贅治療作用、肝炎で代表さ
れる色素沈着症治療作用、尋常性乾癬治療症、老人性乾
皮症、老人性角化腫治療作用、物理的原因による皮膚損
傷治療作用、発毛促進作用、消化液分泌促進作用、発汗
促進作用、便通促進作用、及び利尿作用からなる群から
選ばれる少なくとも一つの作用を改善する作用を有して
おり、これを投与することにより、肌の衰えの防止と改
善、アトピー性皮膚炎の治療と発症・悪化の予防、発毛
の促進と抜け毛の予防、湿疹の改善と悪化の予防、便通
の促進、排尿の促進等の効果が発揮される。The essence improving agent of the present invention can be used as a beautifying agent, atopic dermatitis treatment, dermatitis group represented by eczema, dermatomycosis treatment, wart treatment, and pigmentation represented by hepatitis. Therapeutic action, psoriasis vulgaris treatment, senile xeroderma, senile keratomas treatment, skin damage treatment due to physical causes, hair growth promoting action, digestive juice secretion promoting action, sweat promoting action, promotion of bowel movement It has an action to improve at least one action selected from the group consisting of an action and a diuretic action, and by administering this, it prevents and ameliorates skin deterioration, and treats and develops / exacerbates atopic dermatitis. It has the effects of preventing hair loss, promoting hair growth and hair loss, improving and preventing eczema, preventing bowel movements, promoting bowel movements, and promoting urination.

【００２５】津液改善剤の好ましい投与量は、疾病の種
類や患者の特性によって異なるが、成人一人一日あたり
１〜１００００ｍｇを１回乃至は数回に分けて経口投与
すればよい。The preferred dose of the tsukumo ameliorating agent varies depending on the type of the disease and the characteristics of the patient, but it may be oral administration of 1 to 10,000 mg per adult per day in one or several divided doses.

【００２６】取り分け本発明で注目すべきことは、上記
一般式（Ｉ）で表される化合物及び／又はその生理的に
許容される塩は、経口投与によって肌が美しくなったり
発毛が促進されたりするなど、複数の作用を同時に備え
ることができる点である。すなわち、好ましくは、本発
明の津液改善剤は、美肌作用、アトピー性皮膚炎治療作
用、湿疹で代表される皮膚炎群治療作用、皮膚真菌症治
療作用、疣贅治療作用、肝炎で代表される色素沈着症治
療作用、尋常性乾癬治療症、老人性乾皮症、老人性角化
腫治療作用、物理的原因による皮膚損傷治療作用、発毛
促進作用、消化液分泌促進作用、発汗促進作用、便通促
進作用、及び利尿作用からなる群から選ばれる二以上の
作用を改善する効果を有する。経口投与でこのような作
用を同時に期待しうる物質は未だ知られていない。In particular, it should be noted in the present invention that the compound represented by the above general formula (I) and / or a physiologically acceptable salt thereof can make the skin beautiful and promote hair growth by oral administration. , Etc., and can have a plurality of actions at the same time. That is, preferably, the essence improving agent of the present invention is represented by a skin beautifying effect, a therapeutic effect on atopic dermatitis, a therapeutic effect on a dermatitis group represented by eczema, a therapeutic effect on dermatomycosis, a therapeutic effect on warts, and a hepatitis. Treatment for pigmentation, treatment for psoriasis vulgaris, treatment for senile xerosis, treatment for senile keratoma, treatment for skin damage due to physical causes, hair growth promotion, digestive secretion promotion, sweating promotion, It has the effect of improving two or more actions selected from the group consisting of a bowel movement promoting action and a diuretic action. There is no known substance capable of simultaneously achieving such an effect by oral administration.

【００２７】（２）本発明の経口投与用組成物 本発明の経口投与用組成物は、本発明の上記津液改善剤
を含有することを特徴とする。上記津液改善剤は１種又
は２種以上を含有してもよい。(2) The composition for oral administration of the present invention The composition for oral administration of the present invention is characterized by containing the above-mentioned Tsutsumi improving agent of the present invention. The above-mentioned Tsutsumi improving agent may contain one kind or two or more kinds.

【００２８】経口投与用組成物としては、顆粒剤、散
剤、錠剤、カプセル剤、キャンディー、ガム、グミ等に
加工した食品組成物や医薬組成物が例示できる。好まし
い本発明の津液改善剤の含有量は、食品組成物の場合、
組成物全体に対し０．００１〜５０重量％であり、０．
０１〜２０重量％がより好ましく、０．０１〜１５重量
％が更に好ましい。また、医薬組成物の場合は０．１〜
６０重量％が好ましく、０．５〜５０重量％がより好ま
しく、１〜３０重量％が更に好ましい。Examples of the composition for oral administration include food compositions and pharmaceutical compositions processed into granules, powders, tablets, capsules, candies, gums, gummy gums and the like. The preferred content of the tsukumo improver of the present invention, in the case of a food composition,
0.001 to 50% by weight based on the whole composition;
The content is more preferably from 0.01 to 20% by weight, even more preferably from 0.01 to 15% by weight. Moreover, in the case of a pharmaceutical composition, 0.1 to
It is preferably 60% by weight, more preferably 0.5 to 50% by weight, and still more preferably 1 to 30% by weight.

【００２９】本発明の組成物は、上記津液改善剤以外
に、食品組成物又は医薬品組成物で通常用いられている
任意成分を含有することができる。このような任意成分
としては、医薬組成物であれば、賦形剤、結合剤、被覆
剤、滑沢剤、糖衣剤、崩壊剤、増量剤、矯味矯臭剤、乳
化・可溶化・分散剤、安定剤、ｐＨ調整剤、等張剤等が
例示できる。食品組成物であれば、酸化防止剤、矯味矯
臭剤、増粘剤、乳化安定剤、防腐剤、呈味剤、甘味剤、
酸味剤等が例示できる。これらの任意成分と上記津液改
善剤を常法に従って処理することにより、本発明の組成
物を製造することができる。The composition of the present invention may contain, in addition to the above-mentioned tsutsumi-improving agent, optional components commonly used in food compositions or pharmaceutical compositions. As such an optional component, if it is a pharmaceutical composition, an excipient, a binder, a coating agent, a lubricant, a sugar coating, a disintegrant, a bulking agent, a flavoring agent, an emulsifying / solubilizing / dispersing agent, Examples include stabilizers, pH adjusters, and isotonic agents. If a food composition, antioxidants, flavoring agents, thickeners, emulsion stabilizers, preservatives, flavoring agents, sweeteners,
Sour agents and the like can be exemplified. The composition of the present invention can be produced by treating these optional components and the above-mentioned tsukumo improver according to a conventional method.

【００３０】本発明の組成物は、津液作用の改善に用い
ることができる。具体的には、美肌作用、アトピー性皮
膚炎治療作用、湿疹で代表される皮膚炎群治療作用、皮
膚真菌症治療作用、疣贅治療作用、肝炎で代表される色
素沈着症治療作用、尋常性乾癬治療症、老人性乾皮症、
老人性角化腫治療作用、物理的原因による皮膚損傷治療
作用、発毛促進作用、消化液分泌促進作用、発汗促進作
用、便通促進作用、及び利尿作用からなる群から選ばれ
る作用の改善のために用いることができる。[0030] The composition of the present invention can be used for improving the essence of the juice. Specifically, it has a beautiful skin effect, an atopic dermatitis treatment effect, a dermatitis group treatment effect represented by eczema, a dermatomycosis treatment effect, a wart treatment effect, a hepatitis represented pigmentation treatment effect, vulgaris Psoriasis treatment, senile xeroderma,
For the treatment of senile keratoma, the treatment of skin damage due to physical causes, the promotion of hair growth, the promotion of digestive juice secretion, the promotion of sweating, the promotion of bowel movement, and the improvement of the action selected from the group consisting of diuretic action. Can be used.

【００３１】[0031]

【実施例】以下に、本発明の実施例を説明する。Embodiments of the present invention will be described below.

【００３２】[0032]

【実施例１〜５】 ＜配合例＞表１に示す成分を用い、その処方に従って錠
剤を作成した。即ち、各処方成分をグラッド造粒装置に
秤込み、５０重量部の２０％エタノール水溶液を噴霧し
ながら混合して、粗顆粒を作成した。粗顆粒を４０℃で
４８時間送風乾燥して、打錠機で打錠して２５０ｍｇの
錠剤を得た。尚、表１中の数値の単位は重量部を表す。Examples 1 to 5 <Formulation Examples> Tablets were prepared using the components shown in Table 1 according to the formulation. That is, each prescription component was weighed in a grading granulator, and mixed by spraying 50 parts by weight of a 20% aqueous ethanol solution to prepare coarse granules. The coarse granules were blow-dried at 40 ° C. for 48 hours, and were compressed with a tableting machine to obtain 250 mg tablets. The units of the numerical values in Table 1 represent parts by weight.

【００３３】[0033]

【表１】 [Table 1]

【００３４】[0034]

【実施例６〜１０】 ＜配合例＞表２に示す成分を用いてその処方に従ってキ
ャンディーを作成した。即ち、各処方成分を１２０℃で
加熱溶解し、冷却しながら成形してキャンディーを得
た。尚、表２中の数値の単位は重量部を表す。Examples 6 to 10 <Formulation Examples> Using the components shown in Table 2, candy was prepared according to the formulation. That is, each prescription component was heated and melted at 120 ° C. and molded while cooling to obtain a candy. The units of the numerical values in Table 2 represent parts by weight.

【００３５】[0035]

【表２】 [Table 2]

【００３６】[0036]

【実施例１１〜１５】 ＜配合例＞表３に示す成分を用いてその処方に従ってキ
ャンディーを作成した。即ち、処方成分を１２０℃で加
熱溶解し、冷却しながら成形してキャンディーを得た。
尚、表３中の数値の単位は重量部を表す。Examples 11 to 15 <Examples of Formulation> Using the components shown in Table 3, candy was prepared according to the formulation. That is, the prescription components were heated and melted at 120 ° C. and molded while cooling to obtain a candy.
The units of the numerical values in Table 3 represent parts by weight.

【００３７】[0037]

【表３】 [Table 3]

【００３８】[0038]

【実施例１６】 ＜試験例１：美肌改善作用＞肌荒れに悩む２８〜３９歳
のパネラー１群１０名が、上記実施例１〜３の錠剤（１
ｇ錠）を１日朝晩２回１錠ずつ２ヶ月間のみ、肌荒れの
改善を評価した。評価基準は、非常に改善した（評点
５）〜改善しない（評点０）とした。対照としては、本
発明の津液改善剤を乳糖に置換したものを用いた。結果
を平均評点として表４に示す。これより、本発明の津液
改善剤が内服によって肌荒れを改善する作用を有するこ
と、即ち、美肌作用を有することがわかる。Example 16 <Test Example 1: Beautiful Skin Improving Effect> Ten groups of panelists aged 28 to 39 years old suffering from rough skin,
g tablets) was evaluated twice a day for two months, one tablet twice a day, only for two months. The evaluation criterion was very improved (gradation 5) to not improved (gradation 0). As a control, lactose was used in place of the liquor improving agent of the present invention. The results are shown in Table 4 as average scores. From this, it can be seen that the rubbing liquid improving agent of the present invention has an effect of improving skin roughness by internal use, that is, has a beautiful skin effect.

【００３９】[0039]

【表４】 [Table 4]

【００４０】[0040]

【実施例１７】 ＜試験例２：発毛促進作用＞Ｃ３Ｈマウス１群５匹の背
部を剃毛し、表５に示す検体１０ｍｇを生理食塩水２０
０μｌに溶解又は分散させ経口投与し、その後の毛の生
え方を観察して発毛促進作用を評価した。対照はベヒク
ルの生理食塩水のみとした。評価の基準は、＋＋（評点
４）：対照に比べて著しく早い、＋（評点２）：対照に
比べて早い、±（評点１）：対照に比べてやや早い、−
（評点０）：対照に比べて早くない、とした。結果を平
均評点として表５に示す。これより、本発明の津液改善
剤は発毛促進作用に優れることが判る。Example 17 <Test Example 2: Hair growth promoting action> The back of a group of five C3H mice was shaved, and 10 mg of a sample shown in Table 5 was added to physiological saline 20.
It was dissolved or dispersed in 0 μl and orally administered, and the subsequent hair growth was observed to evaluate the hair growth promoting effect. The control was vehicle saline only. The evaluation criteria are ++ (score 4): significantly earlier than the control, + (score 2): earlier than the control, ± (score 1): slightly earlier than the control, −
(Score 0): Not earlier than control. The results are shown in Table 5 as average scores. From this, it can be seen that the tsukumo improver of the present invention is excellent in hair growth promoting action.

【００４１】[0041]

【表５】 [Table 5]

【００４２】[0042]

【実施例１８】 ＜試験例３：アトピー性皮膚炎に対する作用＞アトピー
性皮膚炎に悩む２１〜３５歳のパネラー１群１０名が、
上記実施例１〜３の錠剤（１ｇ錠）を１日朝晩２回１錠
ずつ２ヶ月間のみ、アトピー性皮膚炎の改善効果を評価
した。評価基準は、非常に改善した（評点５）〜改善し
ない（評点０）とした。対照としては、本発明の津液改
善剤を乳糖に置換したものを用いた。結果を平均評点と
して表６に示す。これより、本発明の津液改善剤が内服
によってアトピー性皮膚炎を改善する作用を有すること
がわかる。Example 18 <Test Example 3: Effect on Atopic Dermatitis> Ten groups of 21 to 35 year old panelists suffering from atopic dermatitis
The improvement effect of atopic dermatitis was evaluated only for the tablets (1 g tablets) of the above Examples 1 to 3 twice a day for 2 months. The evaluation criterion was very improved (gradation 5) to not improved (gradation 0). As a control, lactose was used in place of the liquor improving agent of the present invention. The results are shown in Table 6 as average scores. From this, it can be seen that the tsumugi improver of the present invention has an effect of improving atopic dermatitis by taking it internally.

【００４３】[0043]

【表６】 [Table 6]

【００４４】[0044]

【実施例１９】 ＜試験例４：湿疹改善作用＞湿疹に悩む１７〜２４歳の
パネラー１群１０名が、上記実施例１〜３の錠剤（１ｇ
錠）を１日朝晩２回１錠ずつ２ヶ月間のみ、湿疹の改善
効果を評価した。評価基準は、非常に改善した（評点
５）〜改善しない（評点０）とした。対照としては、本
発明の津液改善剤を乳糖に置換したものを用いた。結果
を平均評点として表７に示す。これより、本発明の津液
改善剤が内服によって湿疹を改善する作用を有すること
がわかる。Example 19 <Test Example 4: Eczema ameliorating effect> Ten panelists, a group of 17-24 year-old panelists suffering from eczema, took the tablets (1 g) of Examples 1-3.
Tablets) was evaluated twice a day, in the morning and evening, one tablet at a time for 2 months only, to evaluate the effect of improving eczema. The evaluation criterion was very improved (gradation 5) to not improved (gradation 0). As a control, lactose was used in place of the liquor improving agent of the present invention. The results are shown in Table 7 as average scores. From this, it can be seen that the tsukutsu improver of the present invention has an effect of improving eczema by taking it internally.

【００４５】[0045]

【表７】 [Table 7]

【００４６】[0046]

【実施例２０】 ＜試験例５：胃液分泌促進作用＞麻酔犬を用いて胃液の
分泌促進作用を評価した。即ち、ペントバルビツールで
麻酔した犬の胃に投与装置付き内視鏡を導入し、検体と
して表８に示す本発明の津液改善剤１０ｍｇを生理食塩
水１０ｍｌに溶解又は分散させて投与し、その前後の胃
液の分泌を観察した。対照は生理食塩水のみを用いた。
評価の基準は、＋＋（評点４）：対照に比べて著しく胃
液分泌が増大、＋（評点２）：対照に比べて胃液分泌が
増大、±（評点１）：対照に比べてやや分泌が増大、−
（評点０）：分泌が対照に比べて増大せず、とした。結
果を表８に示す。これより、本発明の津液改善剤は胃液
分泌促進作用に優れることがわかる。Example 20 <Test Example 5: Gastric secretion promoting action> The gastric secretion promoting action was evaluated using an anesthetized dog. That is, an endoscope with an administration device was introduced into the stomach of a dog anesthetized with a pentobarbitur, and a 10 mg of the tsunami improving agent of the present invention shown in Table 8 was dissolved or dispersed in 10 ml of physiological saline and administered as a specimen. Gastric juice secretion before and after was observed. As a control, only physiological saline was used.
Evaluation criteria are as follows: ++ (score 4): gastric secretion increased significantly compared to control, + (score 2): gastric secretion increased compared to control, ± (score 1): slightly increased compared to control , −
(Score 0): The secretion did not increase compared to the control. Table 8 shows the results. From this, it can be seen that the tsumugi improving agent of the present invention is excellent in gastric secretion promoting action.

【００４７】[0047]

【表８】 [Table 8]

【００４８】[0048]

【実施例２１】 ＜試験例６：便通・排尿の促進作用＞ＩＣＲマウスを代
謝ケージで飼育した。投与群は上記実施例１〜３で得ら
れた組成物を１ｇ／１匹朝夕２回０．５ｇずつ投与し
た。２４時間尿と糞の量をモニターした。コントロール
群は検体を投与しなかった。各サンプル１群１０匹とし
た。検体投与群の尿量の総和をコントロール群の尿量の
総和で除した値（尿量比）と、検体投与群の糞量の総和
をコントロール群の糞量の総和で除した値（糞量比）と
を表９に示す。これより、本発明の一般式（Ｉ）で表さ
れる化合物及び／又はその生理的に許容される塩は、便
通促進作用及び排尿促進作用（利尿作用）に優れること
がわかる。Example 21 <Test Example 6: Promotion of bowel movement and urination> ICR mice were bred in metabolic cages. In the administration group, the compositions obtained in Examples 1 to 3 were administered at a dose of 0.5 g each at 1 g / mouse twice in the morning and evening. Urine and fecal volume were monitored for 24 hours. The control group received no specimen. Each group consisted of 10 animals. The value obtained by dividing the total urine volume of the sample administration group by the total urine volume of the control group (urine volume ratio) and the value obtained by dividing the total fecal volume of the sample administration group by the total fecal volume of the control group (fecal volume) Are shown in Table 9. This indicates that the compound represented by the general formula (I) and / or a physiologically acceptable salt thereof of the present invention is excellent in the bowel movement promoting action and urination promoting action (diuretic action).

【００４９】[0049]

【表９】 [Table 9]

【００５０】[0050]

【発明の効果】本発明によれば、美肌作用、アトピー性
皮膚炎治療作用、湿疹で代表される皮膚炎群治療作用、
皮膚真菌症治療作用、疣贅治療作用、肝炎で代表される
色素沈着症治療作用、尋常性乾癬治療症、老人性乾皮
症、老人性角化腫治療作用、物理的原因による皮膚損傷
治療作用、発毛促進作用、消化液分泌促進作用、発汗促
進作用、便通促進作用、及び排尿促進作用からなる群か
ら選ばれる津液作用を改善する効果を有する津液改善剤
を提供することができる。According to the present invention, a beautiful skin effect, a therapeutic effect on atopic dermatitis, a therapeutic effect on a dermatitis group represented by eczema,
Treatment for dermatomycosis, treatment for warts, treatment for pigmentation such as hepatitis, treatment for psoriasis vulgaris, treatment for senile xeroderma, senile keratoma, treatment for skin damage due to physical causes It is possible to provide a tsumuco-ameliorating agent having an effect of improving a tsumucho effect selected from the group consisting of a hair growth promoting action, a digestive juice secretion promoting action, a sweat promoting action, a bowel movement promoting action, and a urination promoting action.

───────────────────────────────────────────────────── フロントページの続き (51)Int.Cl.6 識別記号 ＦＩ Ａ６１Ｋ 7/00 Ａ６１Ｋ 7/00 Ｃ Ｄ 7/06 ＡＤＤ 7/06 ＡＤＤ 7/48 7/48 31/19 ＡＢＥ 31/19 ＡＢＥ 31/70 ＡＤＡ 31/70 ＡＤＡ (72)発明者 福島 信 神奈川県横浜市戸塚区柏尾町560 ポーラ 化成工業株式会社戸塚研究所内 (72)発明者 稲岡 靖規 神奈川県横浜市神奈川区高島台27番地１ ポーラ化成工業株式会社横浜研究所内 (72)発明者 奥田 剛弘 神奈川県横浜市神奈川区高島台27番地１ ポーラ化成工業株式会社横浜研究所内──────────────────────────────────────────────────の Continued on the front page (51) Int.Cl. 6 Identification code FI A61K 7/00 A61K 7/00 CD 7/06 ADD 7/06 ADD 7/48 7/48 31/19 ABE 31/19 ABE 31/70 ADA 31/70 ADA (72) Inventor Shin Fukushima 560 Kashio-cho, Totsuka-ku, Yokohama-shi, Kanagawa Prefecture Inside Totsuka Research Laboratories (72) Inventor Yasunori Inaoka 27-1, Takashimadai, Kanagawa-ku, Yokohama-shi, Kanagawa (72) Inventor Takehiro Okuda 27-1-1 Takashimadai, Kanagawa-ku, Yokohama-shi, Kanagawa-ken, Yokohama Research Laboratory

Claims (7)

【特許請求の範囲】[Claims] 【請求項１】 下記一般式（Ｉ）で表される化合物及び
／又はその生理的に許容される塩からなる、津液改善
剤。 【化１】 ［式（Ｉ）中、Ｒ1は水酸基又は糖残基を表し、Ｒ2は水
素原子、水酸基、ヒドロキシメチル基又はカルボキシル
基を表し、Ｒ3はメチル基、カルボキシル基又は水素原
子を表す。Ａはカルボニル基又はＣＨ−Ｒ4で表される
基を表す。ここでＲ4は糖残基又は置換基を有してもよ
いアントラニル基を表す。］1. An agent for improving tsunami comprising a compound represented by the following general formula (I) and / or a physiologically acceptable salt thereof. Embedded image [In the formula (I), R 1 represents a hydroxyl group or a sugar residue, R 2 represents a hydrogen atom, a hydroxyl group, a hydroxymethyl group or a carboxyl group, and R 3 represents a methyl group, a carboxyl group or a hydrogen atom. A represents a group represented by a carbonyl group or a CH-R 4. Here, R 4 represents a sugar residue or an anthranyl group which may have a substituent. ] 【請求項２】 一般式（Ｉ）で表される化合物が、下記
一般式（ＩＩ）で表されるエモジン、下記一般式（ＩＩ
Ｉ）で表されるアロエエモジン、下記一般式（ＩＶ）で
表されるライン、下記一般式（Ｖ）で表されるセンノサ
イド、又は下記一般式（ＶＩ）で表されるアロインであ
る、請求項１記載の津液改善剤。 【化２】 【化３】 【化４】 【化５】 【化６】 2. A compound represented by the general formula (I), wherein emodin represented by the following general formula (II):
The aloe-emodin represented by I), the line represented by the following general formula (IV), the sennoside represented by the following general formula (V), or the aloin represented by the following general formula (VI). The rubbing improver according to the above. Embedded image Embedded image Embedded image Embedded image Embedded image 【請求項３】 請求項１又は２記載の津液改善剤を含有
する、経口投与用組成物。3. A composition for oral administration, comprising the tsukumo ameliorating agent according to claim 1 or 2. 【請求項４】 食品である、請求項３記載の組成物。4. The composition according to claim 3, which is a food. 【請求項５】 医薬である、請求項３記載の組成物。5. The composition according to claim 3, which is a medicament. 【請求項６】 津液作用の改善に用いられる、請求項３
〜５のいずれかに記載の組成物。6. The method according to claim 3, which is used for improving a tsufluid action.
The composition according to any one of claims 1 to 5. 【請求項７】 前記津液作用が、美肌作用、アトピー性
皮膚炎治療作用、皮膚炎群治療作用、皮膚真菌症治療作
用、疣贅治療作用、色素沈着症治療作用、尋常性乾癬治
療症、老人性乾皮症、老人性角化腫治療作用、皮膚損傷
治療作用、発毛促進作用、消化液分泌促進作用、発汗促
進作用、便通促進作用、及び利尿作用からなる群から選
ばれる作用である、請求項６記載の組成物。7. The tanning solution is effective for beautifying skin, treating atopic dermatitis, treating dermatitis, treating dermatomycosis, treating warts, treating pigmentation, treating psoriasis vulgaris, and the elderly. Xeroderma sclerosis, senile keratoma treatment action, skin damage treatment action, hair growth promotion action, digestive secretion promotion action, perspiration promotion action, bowel movement promotion action, and an action selected from the group consisting of diuretic action, A composition according to claim 6.
JP27272696A 1996-10-15 1996-10-15 Tsu fluid improving agent and composition for oral administration containing the same Expired - Lifetime JP4049406B2 (en)

Priority Applications (1)

Application Number Priority Date Filing Date Title
JP27272696A JP4049406B2 (en) 1996-10-15 1996-10-15 Tsu fluid improving agent and composition for oral administration containing the same

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
JP27272696A JP4049406B2 (en) 1996-10-15 1996-10-15 Tsu fluid improving agent and composition for oral administration containing the same

Publications (2)

Publication Number Publication Date
JPH10114650A true JPH10114650A (en) 1998-05-06
JP4049406B2 JP4049406B2 (en) 2008-02-20

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Cited By (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2001051044A3 (en) * 2000-01-12 2002-03-28 Medidom Lab Substances for use in treating psoriasis
JP2002255733A (en) * 2001-02-28 2002-09-11 Alps Yakuhin Kogyo Kk Useful material using sennoside extraction residue as active ingredient
WO2002058681A3 (en) * 2001-01-23 2002-12-19 Negma Lerads Use of rhein for preparing a medicine for treating a high level of il-1
WO2004010990A1 (en) * 2002-07-23 2004-02-05 Negma-Lerads Use of a rhein in a therapeutic treatment requiring a rise in the rate of heme oxygenase
WO2006029893A3 (en) * 2004-09-17 2006-10-19 Oystershell Nv Composition for inhibiting or preventing the formation of a biofilm
KR101170279B1 (en) * 2010-01-20 2012-07-31 영남대학교 산학협력단 Pharmaceutical composition for preventing and treating allergic diseases comprising anthraquinone derivatives

Cited By (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2001051044A3 (en) * 2000-01-12 2002-03-28 Medidom Lab Substances for use in treating psoriasis
JP2003519653A (en) * 2000-01-12 2003-06-24 ラボラトワール・メディドム・エスアー Substances for the treatment of psoriasis
US6844365B2 (en) 2000-01-12 2005-01-18 Laboratoire Medidom S.A. Substances for use in treating psoriasis
JP4912554B2 (en) * 2000-01-12 2012-04-11 ラボラトワール・メディドム・エスアー Substances for the treatment of psoriasis
WO2002058681A3 (en) * 2001-01-23 2002-12-19 Negma Lerads Use of rhein for preparing a medicine for treating a high level of il-1
JP2002255733A (en) * 2001-02-28 2002-09-11 Alps Yakuhin Kogyo Kk Useful material using sennoside extraction residue as active ingredient
WO2004010990A1 (en) * 2002-07-23 2004-02-05 Negma-Lerads Use of a rhein in a therapeutic treatment requiring a rise in the rate of heme oxygenase
WO2006029893A3 (en) * 2004-09-17 2006-10-19 Oystershell Nv Composition for inhibiting or preventing the formation of a biofilm
US7691418B2 (en) 2004-09-17 2010-04-06 Oystershell Nv Composition for inhibiting or preventing the formation of a biofilm
KR101170279B1 (en) * 2010-01-20 2012-07-31 영남대학교 산학협력단 Pharmaceutical composition for preventing and treating allergic diseases comprising anthraquinone derivatives

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